Interest of molecular/crystalline dispersions for the determination of solubility curves of drugs into polymers
We present here a method to increase the dissolution rate of drugs into polymers in order to make easier and faster the determination of the solubility curves of these mixtures. The idea is to prepare molecular/crystalline dispersions (MCD) where the drug is dispersed into the polymer, partly at the molecular level and partly in the form of small crystallites. We show that this particular microstructure greatly increases the dissolution rate of crystallites since: (1) The molecular dispersion has a plasticizing effect which greatly increases the molecular mobility in the amorphous matrix. (2) The fine crystallite dispersio...
Source: International Journal of Pharmaceutics - August 24, 2019 Category: Drugs & Pharmacology Source Type: research

Evaluation of manufacturing process parameters causing multilayer tablets delamination
Publication date: 30 October 2019Source: International Journal of Pharmaceutics, Volume 570Author(s): Marco Bellini, Mathias Walther, Roland BodmeierAbstractThe aim of this study was to evaluate the influence of tableting process parameters, i.e. turret rotation speed, pre-compaction and main compaction pressures, and their interactions on layer adhesion of bilayer tablets. The elastic recovery after compaction was used as estimation for the elasticity of the material. Three potential pharmaceutical formulations were evaluated as combinations of immediate (microcrystalline cellulose, lactose, calcium phosphate, pregelatini...
Source: International Journal of Pharmaceutics - August 24, 2019 Category: Drugs & Pharmacology Source Type: research

Novel olive oil phenolic (−)-oleocanthal (+)-xylitol-based solid dispersion formulations with potent oral anti-breast cancer activities
Publication date: 5 October 2019Source: International Journal of Pharmaceutics, Volume 569Author(s): Mohammed H. Qusa, Abu Bakar Siddique, Sami Nazzal, Khalid A. El SayedAbstractEpidemiological studies have compellingly documented the ability of the Mediterranean diet rich in extra-virgin olive oil to reduce the incidence of certain malignancies, and cardiovascular diseases, and slow the Alzheimer’s disease progression. S-(-)-Oleocanthal (OC) was identified as the most bioactive olive oil phenolic with documented anti-inflammatory, anticancer, and anti-Alzheimer’s activities. OC consumption causes irritating se...
Source: International Journal of Pharmaceutics - August 24, 2019 Category: Drugs & Pharmacology Source Type: research

Development, characterization and evaluation of topical methotrexate-entrapped deformable liposome on imiquimod-induced psoriasis in a mouse model
Publication date: 5 October 2019Source: International Journal of Pharmaceutics, Volume 569Author(s): Mahdiyeh Bahramizadeh, Maryam Bahramizadeh, Bita Kiafar, Amir Hossein Jafarian, Amin Reza Nikpoor, Mahdi Hatamipour, Habibollah Esmaily, Zari Rezaeemehr, Shiva Golmohammadzadeh, Seyedeh Alia Moosavian, Mahmoud Reza JafariAbstractThe aim of this study was to prepare and characterize topical methotrexate (MTX) with different percentages (0.05%, 0.1%, 0.25% and 0.5%) entrapped in deformable liposomes using phosphatidylcholine and oleic acid. The effectiveness and sub-acute toxicity of these topical formulations were investigat...
Source: International Journal of Pharmaceutics - August 21, 2019 Category: Drugs & Pharmacology Source Type: research

Using ordered mesoporous silica sba-15 to limit cutaneous penetration and transdermal permeation of organic uv filters
Publication date: Available online 19 August 2019Source: International Journal of PharmaceuticsAuthor(s): André Luis Máximo Daneluti, Francisco Mariano Neto, Nádia Ruscinc, Ingrid Lopes, Maria Valéria Robles Velasco, Jivaldo Do Rosário Matos, André Rolim Baby, Yogeshvar N. KaliaAbstractAvobenzone (AVO), oxybenzone (OXY), and octyl methoxycinnamate (OMC), are widely used UV filters. The aim of this study was to investigate the effect of incorporation in mesoporous silica (SBA-15) on their cutaneous deposition and permeation. Stick formulations containing “free” and &ldqu...
Source: International Journal of Pharmaceutics - August 21, 2019 Category: Drugs & Pharmacology Source Type: research

The key role of straight fluid jet in predicting the drug dissolution from electrospun nanofibers
Publication date: Available online 19 August 2019Source: International Journal of PharmaceuticsAuthor(s): Yaoyao Yang, Tianhao Zhu, ZhePeng Liu, Minyi Luo, Deng-Guang Yu, SW Annie BlighAbstractIn nanopharmaceutics, a robust manipulation of the preparation process and an accurate prediction of the final product size are very important for developing novel nano drug delivery systems. In the present study, for the first time, a process parameter, i.e. the length of the straight fluid jet, L, is correlated with an experimental parameter, i.e. fluid flow rate, F; a nanofiber property, i.e. diameter, D; and the corresponding dru...
Source: International Journal of Pharmaceutics - August 19, 2019 Category: Drugs & Pharmacology Source Type: research

Multi-dose oral abuse deterrent formulation of Loperamide using Hot melt extrusion
Publication date: Available online 16 August 2019Source: International Journal of PharmaceuticsAuthor(s): Pavan Kumar Nukala, Siddhant Palekar, Manali Patki, Yige Fu, Ketan PatelAbstractLoperamide, an over the counter anti-diarrheal drug, also infamously referred to as “poor man's methadone”. Due to the ease of availability and low price, people/patients abuse it by consuming more than 30 tablets to achieve euphoric effect and to combat opioid withdrawal. But supratherapeutic doses of loperamide result in severe respiratory depression, cardiac dysrhythmia and mortality. To address this issue, we developed ...
Source: International Journal of Pharmaceutics - August 18, 2019 Category: Drugs & Pharmacology Source Type: research

Cyclosporine A-loaded UniORV®: Pharmacokinetic and safety characterization
This study aimed to improve pharmacokinetic behavior and reduce safety concern of cyclosporine A (CsA) by UniORV® approach, a new platform for solid dispersion formulation. CsA-loaded UniORV® (UO/CsA) was prepared, and its physicochemical properties were evaluated in terms of droplet size distribution and dissolution. The pharmacokinetic behavior and nephrotoxic potential of orally-dosed CsA samples (10 mg-CsA/kg) were assessed in rats. After re-dispersion of UO/CsA in water, fine droplets were observed, and the mean diameter of droplets was calculated to be 45 nm. The UniORV® approach markedly improved the dis...
Source: International Journal of Pharmaceutics - August 18, 2019 Category: Drugs & Pharmacology Source Type: research

Targeted and MMP-2/9 responsive peptides for the treatment of rheumatoid arthritis
This study establishes adjuvant-induced arthritis (AIA) mouse models and explores the anti-inflammatory efficacy of QAW in AIA mice. To enhance the targeting, responsiveness, and efficacy of QAW to inflammation, QAW (Q) is modified with a cell penetrating peptide (T), a matrix metalloproteases-2/9 (MMP-2/9) digestive peptide (M), and an inflammation targeting peptide-RGD (R). The designed RMTQ demonstrates enhanced delivery to cytoplasm, higher reduction of pro-inflammatory factors, and better efficacy than QAW. The anti-inflammatory efficacy of RMTQ is similar to that of DEX in this study whereas RMTQ treatment shows a hi...
Source: International Journal of Pharmaceutics - August 16, 2019 Category: Drugs & Pharmacology Source Type: research

Stealth functionalization of biomaterials and nanoparticles by CD47 mimicry
Publication date: Available online 14 August 2019Source: International Journal of PharmaceuticsAuthor(s): Seyed Mohammad Gheibi Hayat, Vanessa Bianconi, Matteo Pirro, Amirhossein SahebkarAbstractPolymeric biomaterials and nanoparticles (NPs) have shown a potential to be widely used for medical purposes. Functional limits of their biocompatibility depend on cellular and molecular responses between host and their artificial surfaces. Accordingly, medical devices of polymer biomaterials like endovascular stents, cardiopulmonary bypass circuits, and prostheses, may trigger inflammation or can be rejected by host due to the ind...
Source: International Journal of Pharmaceutics - August 15, 2019 Category: Drugs & Pharmacology Source Type: research

Evaluation of manufacturing process parameters causin7g multilayer tablets delamination
Publication date: Available online 14 August 2019Source: International Journal of PharmaceuticsAuthor(s): Marco Bellini, Mathias Walther, Roland BodmeierAbstractThe aim of this study was to evaluate the influence of tableting process parameters, i.e. turret rotation speed, pre-compaction and main compaction pressures, and their interactions on layer adhesion of bilayer tablets. The elastic recovery after compaction was used as estimation for the elasticity of the material. Three potential pharmaceutical formulations were evaluated as combinations of immediate (microcrystalline cellulose, lactose, calcium phosphate, pregela...
Source: International Journal of Pharmaceutics - August 15, 2019 Category: Drugs & Pharmacology Source Type: research

Interest of molecular / crystalline dispersions for the determination of solubility curves of drugs into polymers
We present here a method to increase the dissolution rate of drugs into polymers in order to make easier and faster the determination of the solubility curves of these mixtures. The idea is to prepare molecular/crystalline dispersions (MCD) where the drug is dispersed into the polymer, partly at the molecular level and partly in the form of small crystallites. We show that this particular microstructure greatly increases the dissolution rate of crystallites since: (1) The molecular dispersion has a plasticizing effect which greatly increases the molecular mobility in the amorphous matrix. (2) The fine crystallite dispersio...
Source: International Journal of Pharmaceutics - August 15, 2019 Category: Drugs & Pharmacology Source Type: research

Applications of Alginate microspheres in therapeutics delivery and cell culture: past, present and future
Publication date: Available online 14 August 2019Source: International Journal of PharmaceuticsAuthor(s): Dinesh Dhamecha, Rachel Movsas, Ugene Sano, Jyothi U. MenonAbstractPolymers are the backbone of pharmaceutical drug delivery. There are several polymers with varying properties available today for use in different pharmaceutical applications. Alginate is widely used in biomedical research due to its attractive features such as biocompatibility, biodegradability, inertness, low cost, and ease of production and formulation. Encapsulation of therapeutic agents in alginate/alginate complex microspheres protects them from e...
Source: International Journal of Pharmaceutics - August 15, 2019 Category: Drugs & Pharmacology Source Type: research

Tacrolimus-loaded lecithin-based nanostructured lipid carrier and nanoemulsion with propylene glycol monocaprylate as a liquid lipid: formulation characterization and assessment of dermal delivery compared to referent ointment
Publication date: Available online 13 August 2019Source: International Journal of PharmaceuticsAuthor(s): Vedrana Savić, Tanja Ilić, Ines Nikolić, Bojan Marković, Bojan Čalija, Nebojša Cekić, Snežana SavićAbstractNanostructured lipid carriers (NLC) and nanoemulsions (NE) are colloid carriers which could improve dermal delivery of tacrolimus. The aims of this study were to evaluate effects of different formulation and process parameters on physicochemical characteristics and stability of lecithin-based NLC with glyceryl palmitostearate as solid and propylene glycol monocaprylate as liquid lipid and to compare...
Source: International Journal of Pharmaceutics - August 15, 2019 Category: Drugs & Pharmacology Source Type: research

Developement, characterization and evaluation of topical methotrexate-entrapped deformable liposome on imiquimod-induced psoriasis in a mouse model
Publication date: Available online 13 August 2019Source: International Journal of PharmaceuticsAuthor(s): Mahdiyeh Bahramizadeh, Maryam Bahramizadeh, Bita Kiafar, Amir Hossein Jafarian, Amin Reza Nikpoor, Mahdi Hatamipour, Habibollah Esmaily, Zari Rezaeemehr, Shiva Golmohammadzadeh, Seyedeh Alia Moosavian, Mahmood Reza JafariAbstractThe aim of this study was to prepare and characterize topical methotrexate (MTX) with different percentages (0.05%, 0.1%, 0.25% and 0.5%) entrapped in deformable liposomes using phosphatidylcholine and oleic acid. The effectiveness and sub-acute toxicity of these topical formulations were inves...
Source: International Journal of Pharmaceutics - August 15, 2019 Category: Drugs & Pharmacology Source Type: research

Controlled release of doxorubicin from polyethylene glycol functionalized melanin nanoparticles for breast cancer therapy: Part I. Production and drug release performance of the melanin nanoparticles
In this study, polyethylene glycol (PEG) conjugated melanin nanoparticles (MNPs) were prepared (PEG-MNPs). A model chemotherapy drug, doxorubicin (DOX), was loaded into the PEG-MNPs with varied concentrations (0.125, 0.250, 0.500 mg/mL). TEM images showed that, DOX-PEG-MNPs are spherical-shaped and 15±2.2 nm in diameter. FTIR spectroscopy analysis demonstrated that MNPs were successfully modified with PEG. The UV-Vis spectroscopy results showed that the drug loading capacity of MNPs was 0.7 mg/ml of DOX in 2 mg/ml of PEG-MNPs. The time course data showed that, the release behavior of DOX from MNPs was primarily diff...
Source: International Journal of Pharmaceutics - August 14, 2019 Category: Drugs & Pharmacology Source Type: research

Stabilization of HSV-2 Viral Vaccine Candidate by Spray Drying
Publication date: Available online 12 August 2019Source: International Journal of PharmaceuticsAuthor(s): Daniel A. LeClair, Lillian Li, Nausheen Rahman, Emily D. Cranston, Zhou Xing, Michael R. ThompsonAbstractThis work demonstrates that an HSV-2 candidate vaccine can be thermostabilized by spray drying to reduce cold chain demands. This work is also to optimize the process responses by varying spray dry parameters for pre-screened suitable excipients; and to determine the validity of current prescreening techniques. Vaccine activity losses were measured by in vitro plaque forming assay with Vero cell line. An accelerated...
Source: International Journal of Pharmaceutics - August 14, 2019 Category: Drugs & Pharmacology Source Type: research

Key determinants of siRNA delivery mediated by unique pH-responsive lipid-based liposomes
Publication date: Available online 12 August 2019Source: International Journal of PharmaceuticsAuthor(s): Mariko Sako, Furan Song, Ayaka Okamoto, Hiroyuki Koide, Takehisa Dewa, Naoto Oku, Tomohiro AsaiAbstractLipid-based nanoparticles, a potential nonviral vector due to their good biocompatibility and biodegradability, have been extensively developed for the delivery of small interfering RNA (siRNA). We designed a unique pH-responsive lipid derivative, a dioleylphosphate-diethylenetriamine conjugate (DOP-DETA). DOP-DETA consists of a pH-responsive triamine and unsaturated fatty acids that accelerate membrane fusion. Our re...
Source: International Journal of Pharmaceutics - August 14, 2019 Category: Drugs & Pharmacology Source Type: research

Drug stabilization in the gastrointestinal tract and potential applications in the colonic delivery of oral zein-based formulations
Publication date: Available online 12 August 2019Source: International Journal of PharmaceuticsAuthor(s): Phuong H.L. Tran, Wei Duan, Beom-Jin Lee, Thao T.D. TranAbstractIn recent years, various oral dosage forms using biomaterials have been developed to deliver drugs to the colon for therapy due to the advantages of local treatment and its ideal location for drug delivery. To achieve site-specific delivery, the complete drug should be released in the colon, while the drug must be protected or their delivery minimized in the stomach and small intestine. The use of natural or synthetic polymers has been reported for these p...
Source: International Journal of Pharmaceutics - August 14, 2019 Category: Drugs & Pharmacology Source Type: research

Development of an optimized freeze-drying protocol for OM-PBAE nucleic acid polyplexes
Publication date: Available online 12 August 2019Source: International Journal of PharmaceuticsAuthor(s): C. Fornaguera, C. Castells-Sala, M.A. Lázaro, A. Cascante, S. BorrósAbstractLong-term stability of polyplexes used for biomedical purposes is an objective envisaged by any research group developing this kind of nanoformulations. However, since biodegradable polymers such as oligopeptide end-modified poly (β-aminoester) (OM-PBAE) are frequently used to ensure safety, and formulations are produced as aqueous dispersions, the stability of the nanoformulations is usually compromised. In this context, fre...
Source: International Journal of Pharmaceutics - August 14, 2019 Category: Drugs & Pharmacology Source Type: research

Mass-Customization of Oral Tablets via the Combination of 3D Printing and Injection Molding
Publication date: Available online 12 August 2019Source: International Journal of PharmaceuticsAuthor(s): Evert Fuenmayor, Crevan O'Donnell, Noel Gately, Patrick Doran, Declan M. Devine, John G. Lyons, Christopher McConville, Ian MajorAbstractThe new frontier of medicine is the personalization of treatment to match a patient’s individual needs. Fused-filament fabrication (FFF) offers a platform for the personalization of drug dosage forms, but one of its chief shortcomings compared to other tablet production methods such as dry compression and wet granulation is relatively low throughput. Conversely, injection moldin...
Source: International Journal of Pharmaceutics - August 14, 2019 Category: Drugs & Pharmacology Source Type: research

Evaluation of Co-delivery of Colistin and Ciprofloxacin in Liposomes Using an In Vitro Human Lung Epithelial Cell Model
This study demonstrated that co-delivery of colistin and ciprofloxacin in a single liposome can reduce transport capacity of both drugs across the lung epithelial cell monolayer and enhance drug retention on the lung epithelial surfaces; therefore, it is a promising approach to treat the respiratory infections caused by multidrug resistant Pseudomonas aeruginosa.Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - August 14, 2019 Category: Drugs & Pharmacology Source Type: research

Protein-Protein Interactions and Water Activity Coefficients can be used to aid a first Excipient Choice in Protein Formulations
Publication date: Available online 12 August 2019Source: International Journal of PharmaceuticsAuthor(s): Miko Schleinitz, Gabriele Sadowski, Christoph BrandenbuschAbstractWith respect to all biopharmaceuticals marketed to date, monoclonal antibodies represent the largest fraction with more than 48% market share (2012). However, the development of biopharmaceutical formulations is a challenging task, and time-consuming and cost-intensive high-throughput screenings are still state-of-the-art in formulation design. These screening techniques are almost exclusively based on heuristic decisions thus the benefit in terms of mec...
Source: International Journal of Pharmaceutics - August 14, 2019 Category: Drugs & Pharmacology Source Type: research

A solid lipid nanoparticle formulation of 4-(N)-docosahexaenoyl 2′, 2′-difluorodeoxycytidine with increased solubility, stability, and antitumor activity
Publication date: Available online 12 August 2019Source: International Journal of PharmaceuticsAuthor(s): Solange A. Valdes, Riyad F. Alzhrani, Andres Rodriguez, Dharmika S.P. Lansakara-P, Sachin G. Thakkar, Zhengrong CuiAbstractPreviously, we synthesized 4-(N)-docosahexaenoyl 2′, 2′-difluorodeoxycytidine (DHA-dFdC), a novel lipophilic compound with a potent, broad-spectrum antitumor activity. Herein, we report a solid lipid nanoparticle (SLN) formulation of DHA-dFdC with improved apparent aqueous solubility, chemical stability, as well as efficacy in a mouse model. The SLNs were prepared from lecithin/glycerol...
Source: International Journal of Pharmaceutics - August 14, 2019 Category: Drugs & Pharmacology Source Type: research

Topical iontophoresis of buflomedil hydrochloride increases drug bioavailability in the mucosa: A targeted approach to treat oral submucous fibrosis
Publication date: Available online 12 August 2019Source: International Journal of PharmaceuticsAuthor(s): Vasundhara Tyagi, Sergio del-Rio Sancho, Maria Lapteva, Yogeshvar N. KaliaAbstractThe aim was to investigate the effect of constant current iontophoresis on the delivery and biodistribution of buflomedil hydrochloride (BUF) in the buccal mucosa. Quantification was by UHPLC-MS/MS; in addition to total delivery, the amounts present in the epithelia and the lamina propria (the target tissue) were also determined. Two-compartment vertical diffusion cells were used to investigate the effect of current density (0.5, 1 and 2 ...
Source: International Journal of Pharmaceutics - August 12, 2019 Category: Drugs & Pharmacology Source Type: research

Quantitative evaluation of the thallium binding of soluble and insoluble Prussian blue hexacyanoferrate analogs: A scientific comparison based on their critical quality attributes
In conclusion, it is essential that the FDA approved iron form with well-defined CQAs is used to treat thallium poisoning and radioactive thallium metal contamination for consistent therapeutic outcomes.Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - August 9, 2019 Category: Drugs & Pharmacology Source Type: research

How tenofovir disoproxil fumarate can impact on solubility and dissolution rate of efavirenz?
Publication date: Available online 8 August 2019Source: International Journal of PharmaceuticsAuthor(s): Giovana Carolina Bazzo, Dina Mostafa, Maria Terezinha França, Bianca Ramos Pezzini, Hellen Karine StulzerAbstractEfavirenz (EFZ) and tenofovir disoproxil fumarate (TDF) can be used simultaneously in the treatment of human immunodeficiency virus type-1 infection. In this work the impact of TDF, a hydrophilic drug, on the solubility and dissolution rate of EFZ, a poorly water-soluble drug, was evaluated. EFZ/TDF binary mixtures in different molar ratios were prepared. Differential scanning calorimetry (DSC) results...
Source: International Journal of Pharmaceutics - August 9, 2019 Category: Drugs & Pharmacology Source Type: research

Treatment of endotoxin-induced uveitis by topical application of cyclosporine a-loaded PolyGel™ in rabbit eyes
Publication date: 5 October 2019Source: International Journal of Pharmaceutics, Volume 569Author(s): Aws Alshamsan, Mohd Abul Kalam, Mohammad Reza Vakili, Ziyad Binkhathlan, Mohammad Raish, Raisuddin Ali, Turki A. Alturki, Nazila Safaei Nikouei, Afsaneh LavasanifarAbstractThe main objective of this study was to investigate the potential of poly(α-carboxylate-co-α-benzylcarboxylate-ε-caprolactone)-block-poly(ethylene glycol)-block-poly(α-carboxylate-co-α-benzylcarboxylate-ε-caprolactone) (PCBCL-b-PEG-b-PCBCL; denoted as PolyGel™) as an in situ gel system for ocular delivery of C...
Source: International Journal of Pharmaceutics - August 9, 2019 Category: Drugs & Pharmacology Source Type: research

EGFR-targeted immunoliposomes as a selective delivery system of simvastatin, with potential use in treatment of triple-negative breast cancers
Publication date: Available online 7 August 2019Source: International Journal of PharmaceuticsAuthor(s): Lucyna Matusewicz, Beata Filip-Psurska, Mateusz Psurski, Sabina Tabaczar, Joanna Podkalicka, Joanna Wietrzyk, Piotr Ziółkowski, Aleksander Czogalla, Aleksander F. SikorskiAbstractA promising strategy for treatment of EGFR-dependent tumours is EGFR signal transduction suppression via inhibition of HMG-CoA reductase using high doses of statins, popular cholesterol-lowering drugs.The main purpose of this study was to obtain (tLCLS) with anti-EGFR antibody attached to their surface and to test whether they can be ef...
Source: International Journal of Pharmaceutics - August 8, 2019 Category: Drugs & Pharmacology Source Type: research

Evaluation of size-based distribution of drug and excipient in amphotericin B liposomal formulation
The objective of this study is to develop an analytical method which can separate the liposomes into different sizes and obtain information of the drug and excipient distribution in the different sized liposomes. We developed an asymmetric flow field-flow fractionation (AF4) method for size-based separation of AmBisome, an amphotericin B liposomal formulation, and a high-performance liquid chromatography ultraviolet-visible and charged aerosol detection (HPLC-UV-CAD) method for simultaneous quantitation of the API (Amphotericin B) and the lipid excipients [1,2-Distearoyl-sn-glycero-3-phosphoglycerol (DSPG), hydrogenated so...
Source: International Journal of Pharmaceutics - August 8, 2019 Category: Drugs & Pharmacology Source Type: research

Electrospun amorphous solid dispersions of meloxicam: influence of polymer type and downstream processing to orodispersible dosage forms
The objectives of this work were to develop meloxicam based amorphous solid dispersion through electrospinning technique and evaluate the effect of the polymeric matrix on the physicochemical properties of the fibers and the downstream processing ability to orodispersible dosage forms. Drug – polymer interactions formed between Eudragit E and meloxicam, confirmed through Raman and 1HNMR spectra, enabled the development of fibers from ethanol, thus allowing an increased production rate compared to PVPk30 where a DMF:THF solvent system was suitable. Microflux dissolution-permeation studies showed a significantly higher...
Source: International Journal of Pharmaceutics - August 7, 2019 Category: Drugs & Pharmacology Source Type: research

Introducing article numbering to International Journal of Pharmaceutics
Publication date: 10 September 2019Source: International Journal of Pharmaceutics, Volume 568Author(s): (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - August 7, 2019 Category: Drugs & Pharmacology Source Type: research

Development and in vitro evaluation of an abuse-deterrent formulation based on a crosslinked starch derivative
Publication date: Available online 5 August 2019Source: International Journal of PharmaceuticsAuthor(s): Rand Ahmad, Hamid OmidianAbstractAn innovative abuse-deterrent composition was developed to deter the most dangerous route of drug abuse, the intravenous route. The composition is based on a crosslinked sodium starch glycolate (X-SSG) that can effectively complex with cationic drugs in aqueous solutions and minimize the amount of the free drug available for extraction. Furthermore, the crosslinked polymer swells in and entraps a portion of the drug solution by which it reduces the available volume for syringing and subs...
Source: International Journal of Pharmaceutics - August 6, 2019 Category: Drugs & Pharmacology Source Type: research

Evaluation iontophoretic delivery of a cationic ketoprofen prodrug for treating nociceptive symptoms in monosodium iodoacetate induced osteoarthritic rat model
Publication date: Available online 5 August 2019Source: International Journal of PharmaceuticsAuthor(s): Shabbir Lobo, Guang YanAbstractTopical nonsteroidal anti-inflammatory drugs have been used in treatment of osteoarthritis but their efficacy is marginal. One major reason is because of limited drug direct penetration to affected joint and muscle tissues from the topical application. The main purpose of this study was to evaluate a new topical treatment through enhancing the direct drug penetration to local muscle and joint tissues for improving topical treatment of osteoarthritis. A cationic prodrug, ketoprofen choline ...
Source: International Journal of Pharmaceutics - August 6, 2019 Category: Drugs & Pharmacology Source Type: research

PEGylated AgNP covered with cationic carbosilane dendrons to enhance antibacterial and inhibition of biofilm properties
Publication date: Available online 5 August 2019Source: International Journal of PharmaceuticsAuthor(s): Andrea Barrios-Gumiel, Javier Sanchez-Nieves, Jorge Pérez-Serrano, Rafael Gómez, F. Javier de la MataAbstractThis work focuses on preparation of silver nanoparticles (AgNP) covered with cationic carbosilane dendrons and poly(ethylene glycol) (PEG). It is well known that AgNP and cationic carbosilane dendritic systems present antibacterial properties. On the other hand, PEG ligand provides antifouling properties and improved biocompatibility. Hence, combination of both ligands, carbosilane dendrons and PEG,...
Source: International Journal of Pharmaceutics - August 6, 2019 Category: Drugs & Pharmacology Source Type: research

Targeted Cancer Treatment Using a Combination of siRNA-Liposomes and Resveratrol-Electrospun Fibers in Co-Cultures
In this study, we evaluated a novel combination of drug delivery devices composed of holo-transferrin conjugated liposomes for siRNA (36 nM) delivery, and electrospun polycaprolactone (PCL)-gelatin (GT) microfibers for resveratrol (40 µM) release. Single- and co-cultures of cancerous K562 cells and human umbilical vein endothelial cells (HUVECs) were used to test the efficacy and targeting over eight days. BCR-ABL siRNA-encapsulated (36 nM) holo-transferrin-conjugated PEG-liposomes were characterized using dynamic light scattering, and transmission electron microscopy. RT-qPCR was performed to assess the silencing BC...
Source: International Journal of Pharmaceutics - August 6, 2019 Category: Drugs & Pharmacology Source Type: research

RNA-based Therapy for Osteogenesis
Publication date: Available online 5 August 2019Source: International Journal of PharmaceuticsAuthor(s): Pinpin Wang, Federico Perche, Delphine Logeart-Avramoglou, Chantal PichonAbstractNucleic acid-based therapy has shown great promise in accelerating bone regeneration as well as other diseases. Nucleic acids used in gene therapy mainly are either plasmid DNA (pDNA) or RNAs. Although pDNA therapy has been extensively studied for decades with encouraging preclinical and clinical results, side effects, and low efficiency associated with nuclear trafficking are hard to bypass. Unlike pDNA, RNAs (mRNA, siRNA, miRNA) exert the...
Source: International Journal of Pharmaceutics - August 6, 2019 Category: Drugs & Pharmacology Source Type: research

Novel Olive Oil Phenolic (-)-Oleocanthal (+)-Xylitol-Based Solid Dispersion Formulations with Potent Oral Anti-Breast Cancer Activities
Publication date: Available online 5 August 2019Source: International Journal of PharmaceuticsAuthor(s): Mohammed H. Qusa, Abu Bakar Siddique, Sami Nazzal, Khalid A. El SayedAbstractEpidemiological studies have compellingly documented the ability of the Mediterranean diet rich in extra-virgin olive oil to reduce the incidence of certain malignancies, and cardiovascular diseases, and slow the Alzheimer’s disease progression. S-(-)-Oleocanthal (OC) was identified as the most bioactive olive oil phenolics with documented anti-inflammatory, anticancer, and anti-Alzheimer’s activities. OC consumption causes irritati...
Source: International Journal of Pharmaceutics - August 6, 2019 Category: Drugs & Pharmacology Source Type: research

Computer-based formulation design and optimization using Hansen Solubility Parameters to enhance the delivery of ibuprofen through the skin
Publication date: Available online 5 August 2019Source: International Journal of PharmaceuticsAuthor(s): Bshaer M. Jameel, An Huynh, Aastha Chadha, Sujata Pandey, Jacalyn Duncan, Mark Chandler, Gabriella BakiAbstractTrial-and-error approach to formulation development is long and costly. With growing time and cost pressures in the pharmaceutical industry, the need for computer-based formulation design is greater than ever. In this project, emulgels were designed and optimized using Formulating for EfficacyTM (FFE) for the topical delivery of ibuprofen. FFE helped select penetration enhancers, design and optimize emulgels an...
Source: International Journal of Pharmaceutics - August 6, 2019 Category: Drugs & Pharmacology Source Type: research

Stability of lyophilized albumin formulations: Role of excipient crystallinity and molecular mobility
Publication date: 5 October 2019Source: International Journal of Pharmaceutics, Volume 569Author(s): Sampreeti Jena, N.S. Krishna Kumar, Alptekin Aksan, Raj SuryanarayananAbstractIn freeze-dried protein formulations, the composition governs the physical forms of the excipients and hence their functionality. It is also necessary to understand the effect of composition on the molecular relaxation behavior, a key factor influencing protein stability. Mannitol (bulking agent) – trehalose (lyoprotectant) – bovine serum albumin (BSA) lyophiles with varying trehalose to BSA mass ratios were investigated. The crystalli...
Source: International Journal of Pharmaceutics - August 6, 2019 Category: Drugs & Pharmacology Source Type: research

Improving the hypoglycemic effect of insulin via the nasal administration of deep eutectic solvents
In conclusion, CM-DES showed promising potential in enhancing the hypoglycemic effect of insulin via the nasal route.Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - August 6, 2019 Category: Drugs & Pharmacology Source Type: research

Spray-Dried Anti-Campylobacter Bacteriophage CP30A Powder Suitable for Global Distribution without Cold Chain Infrastructure
In this study, a spray drying and packaging process was developed to produce a thermally-stable dry powder containing bacteriophages that retains biological activity against C. jejuni after long distance shipping at ambient temperature. Spray drying using a twin-fluid atomizer resulted in significantly less (p
Source: International Journal of Pharmaceutics - August 5, 2019 Category: Drugs & Pharmacology Source Type: research

Construction and in vitro and in vivo evaluation of folic acid-modified nanostructured lipid carriers loaded with paclitaxel and chlorin e6
Publication date: Available online 5 August 2019Source: International Journal of PharmaceuticsAuthor(s): Qibo Zhang, Jihui Zhao, Hongmei Hu, Yulu Yan, Xiaoge Hu, Kuan Zhou, Sirui Xiao, Yongtai Zhang, Nianping FengAbstractBreast cancer remains a major threat to women’s health, and the incidence of breast cancer continues to increase each year. Paclitaxel (PTX) is commonly used to treat breast cancer, but shows limited solubility and is associated with major side effects, limiting its clinical applications. Photodynamic therapy (PDT) is a promising treatment for breast cancer but is limited by the poor solubility of ph...
Source: International Journal of Pharmaceutics - August 5, 2019 Category: Drugs & Pharmacology Source Type: research

Degradable, thermo-, pH- and redox-sensitive hydrogel microcapsules for burst and sustained release of drugs
Publication date: Available online 3 August 2019Source: International Journal of PharmaceuticsAuthor(s): Marcin Mackiewicz, Jan Romanski, Kinga Drabczyk, Ewelina Waleka, Zbigniew Stojek, Marcin KarbarzAbstractPolymer microcapsules offer a possibility of storing increased amounts of drugs. Appropriate design and composition of the microcapsules allow tuning of the drug-release process. In this paper, we report on synthesis of hydrogel microcapsules sensitive to temperature and pH and degradable by glutathione and hydrogen peroxide. Microcapsules were based on thermo-responsive poly(N-isopropylacrylamide) and degradable cyst...
Source: International Journal of Pharmaceutics - August 4, 2019 Category: Drugs & Pharmacology Source Type: research

Novel lavender oil and silver nanoparticles simultaneously loaded onto polyurethane nanofibers for wound-healing applications
In this study, a novel technique was used to fabricate composite electrospun wound-dressing nanofibers composed of polyurethane encasing lavender oil and silver (Ag) nanoparticles (NPs). After electrospinning, the fabricated nanofibers were identified using various techniques, including scanning electron microscopy (SEM) and transmission electron microscopy (TEM). An abundance of Ag NPs in the fibers decreased the diameter of the fibers while increased concentration of the lavender oil increased the diameter. Fourier transform infrared (FTIR) and X-ray diffraction (XRD) studies showed the presence of the lavender oil and A...
Source: International Journal of Pharmaceutics - August 4, 2019 Category: Drugs & Pharmacology Source Type: research

Modified chitosan-based nanoadjuvants enhance immunogenicity of protein antigens after mucosal vaccination
Publication date: Available online 3 August 2019Source: International Journal of PharmaceuticsAuthor(s): Genada Sinani, Melike Sessevmez, M. Koray Gök, Saadet Özgümüş, H. Oya Alpar, Erdal CevherAbstractNasal vaccination is considered to be an effective and convenient way of increasing immune responses both systemically and locally. Although various nanovaccine carriers have been introduced as potential immune adjuvants, further improvements are still needed before they can be taken to clinical usage. Chitosan-based nanovaccine carriers are one of the most widely studied adjuvants, owing ...
Source: International Journal of Pharmaceutics - August 4, 2019 Category: Drugs & Pharmacology Source Type: research

Physiologically based mathematical modelling of solute transport within the epidermis and dermis
Publication date: Available online 1 August 2019Source: International Journal of PharmaceuticsAuthor(s): Joshua J. Calcutt, Yuri G. AnissimovAbstractThe stratum corneum is the main barrier to transdermal drug delivery which has previously resulted in mathematical modelling of solute transport in the skin being primarily directed at this skin layer. However, for topical treatment and skin toxicity studies, the concentration in the epidermis and dermis is important and needs to be modelled mathematically. Hitherto, mathematical models for viable skin layers typically simplified the clearance of solute by blood, either assumi...
Source: International Journal of Pharmaceutics - August 2, 2019 Category: Drugs & Pharmacology Source Type: research

Pectin-based (LA-co-MAA) Semi-IPNS as a Potential Biomaterial for Colonic Delivery of Oxaliplatin
This study describes the fabrication of chemically crosslinked pectin-based LA-co-MAA hydrogels through free radical polymerization technique for the colonic delivery of oxaliplatin. Methylene bisacrylamide was used as a crosslinking agent and ammonium persulfate as an initiator. The successful fabrication and drug loading were confirmed through Fourier transform infrared spectroscopy (FTIR). The thermal investigations through differential scanning calorimetry (DSC) and thermogravimetric analysis (TGA) suggested the higher thermal stability of the unloaded and OXP-loaded formulations as compared to the raw materials. X-ray...
Source: International Journal of Pharmaceutics - August 2, 2019 Category: Drugs & Pharmacology Source Type: research

Assessment of volumetric scale-up law for processing of a sustained release formulation on co-rotating hot-melt extruders
Publication date: Available online 1 August 2019Source: International Journal of PharmaceuticsAuthor(s): Jeroen Van Renterghem, Shana Van De Steene, Tryfon Digkas, Margarethe Richter, Chris Vervaet, Thomas De BeerAbstractIn this research, the volumetric scale-up law was assessed for its applicability to scale-up from a laboratory-scale extruder (11 mm diameter) to a pilot-scale extruder (16 mm diameter) with geometric similarity using low feed rates (0.1-0.26 kg/h at lab-scale). A sustained release formulation was extruded on both scales using scaled feed rates according to the volumetric scale-up law. The specific mechani...
Source: International Journal of Pharmaceutics - August 2, 2019 Category: Drugs & Pharmacology Source Type: research

Improved self-assembled micelles based on supercritical fluid technology as a novel oral delivery system for enhancing germacrone oral bioavailability
Publication date: Available online 1 August 2019Source: International Journal of PharmaceuticsAuthor(s): Xuefeng Hou, Beibei Cao, Yuanzhi He, Teng Guo, Zhe Li, Ying Liu, Yongtai Zhang, Nianping FengAbstractThe main objective of this study was to develop a novel self-assembled micelle system to improve the oral bioavailability of the water-insoluble and thermal instable germacrone (GEM). Micelles were prepared with an improved supercritical reverse phase evaporation (ISCRPE) method, and the thin-film hydration (TFH) method was used for comparison. Physicochemical characterization confirmed the nanospherical morphology of th...
Source: International Journal of Pharmaceutics - August 2, 2019 Category: Drugs & Pharmacology Source Type: research